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    • 16. 发明授权
    • Tertiary-butyldimethylsilyl carbamate derivative and process for
producing the same
    • 叔丁基二甲基甲硅烷基氨基甲酸酯衍生物及其制备方法
    • US4837349A
    • 1989-06-06
    • US909397
    • 1986-09-19
    • Yasufumi OhfuneMasahiro Sakaitani
    • Yasufumi OhfuneMasahiro Sakaitani
    • C07F7/18
    • C07F7/1896
    • A t-butyldimethylsilyl carbamate derivative and a process for producing the same are disclosed. Tertiary-butyldimethylsilyl carbamate derivatives having the following general formula (1) are intermediates for the production of a variety of carbamate esters that can be extensively used as drugs acting on the central nervous system or circulatory organs, as agrichemicals (e.g. insecticides and herbicides), or as antimicrobial agents; a process capable of economical and efficient production of such intermediates is also disclosed: ##STR1## where R.sup.1 is an alkyl group having 1-3 carbon atoms or a hydrogen atom; R.sup.2 is ##STR2## (where R.sup.3 is a hydrogen atom, an alkyl, alkenyl or aralkyl group having 1-10 carbon atoms, each of which groups may be substituted by a hydroxyl group, a t-butyldimethylsilyloxy group, a methylthio group, a lower alkoxycarbonyl group, a lower alkoxy group, an indolyl group or an imidazolyl group; R.sup.4 is a lower alkoxycarbonyl group, an N-alkylamido group having 2-6 carbon atoms, an O-tetrahydropyranylthr eonine methyl ester amido residue, an O-t-butyldimethylsilylthreonine methyl ester amido residue, a threonine methyl ester amido residue or --(CH.sub.2).sub.n --COOR.sup.5 (where n is an integer of 1-3 and R.sup.5 is a lower alkyl group), provided that R.sup.3 combines with R.sup.4 to form a cyclopentyl group, a cyclohexyl group, a tetrahydrofuranyl group or a dioxanyl group, these rings being optionally substituted by a lower alkyl group, a lower alkenyl group, a lower alkoxycarbonyl group or a lower alkoxycarbonylmethyl group); and R.sup.1 and R.sup.2, when taken together, form a 4- or 5-membered carbon ring, which may be substituted by a lower alkoxycarbonyl group or a t-butyldimethylsilyloxycarbonyl group.
    • 公开了一种叔丁基二甲基甲硅烷基氨基甲酸酯衍生物及其制备方法。 具有以下通式(1)的叔丁基二甲基甲硅烷基氨基甲酸酯衍生物是用于生产可广泛用作作为农药(例如杀虫剂和除草剂)作为中枢神经系统或循环器官的药物的各种氨基甲酸酯的中间体, 或作为抗微生物剂; 还公开了能够经济有效地生产这样的中间体的方法:其中R1是具有1-3个碳原子的烷基或氢原子的(1) R2是(其中R3是氢原子,具有1-10个碳原子的烷基,烯基或芳烷基,它们各自可以被羟基取代,叔丁基二甲基甲硅烷氧基,甲硫基, 低级烷氧基羰基,低级烷氧基,吲哚基或咪唑基; R4为低级烷氧基羰基,具有2-6个碳原子的N-烷基酰氨基,O-四氢吡喃基硫代氨基甲酸酯酰胺残基,二叔丁基二甲基甲硅烷基苏氨酸 甲基酯酰氨基残基,苏氨酸甲酯酰氨基残基或 - (CH 2)n -COOR 5(其中n为1-3的整数,R 5为低级烷基),条件是R 3与R 4结合形成环戊基, 环己基,四氢呋喃基或二恶烷基,这些环任选被低级烷基,低级烯基,低级烷氧基羰基或低级烷氧基羰基甲基取代)。 当R 1和R 2一起形成可被低级烷氧基羰基或叔丁基二甲基甲硅烷氧基羰基取代的4-或5-元碳环时,